| Reaction Details |
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 | Report a problem with these data |
| Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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| Ligand | BDBM107767 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1690806 (CHEMBL4041376) |
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| IC50 | 1.000000±n/a nM |
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| Citation |  Mikami, S; Nakamura, S; Ashizawa, T; Nomura, I; Kawasaki, M; Sasaki, S; Oki, H; Kokubo, H; Hoffman, ID; Zou, H; Uchiyama, N; Nakashima, K; Kamiguchi, N; Imada, H; Suzuki, N; Iwashita, H; Taniguchi, T Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem60:7677-7702 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| cGMP-dependent 3',5'-cyclic phosphodiesterase |
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| Name: | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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| Synonyms: | CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | Homo sapiens phosphodiesterase 2A (PDE2A) | NM_002599 | PDE2A | PDE2A_HUMAN | cGSPDE |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 105691.58 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O00408 |
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| Residue: | 941 |
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| Sequence: | MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
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| BDBM107767 |
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| n/a |
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| Name | BDBM107767 |
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| Synonyms: | US11419874, PF-05180999 | US8598155, 2 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H17F3N8 |
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| Mol. Mass. | 414.3871 |
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| SMILES | Cc1nc(-c2cnn(C)c2-c2ccc(cn2)C(F)(F)F)c2c(ncnn12)N1CCC1 |
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| Structure | 
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